JP2013535460A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013535460A5 JP2013535460A5 JP2013521139A JP2013521139A JP2013535460A5 JP 2013535460 A5 JP2013535460 A5 JP 2013535460A5 JP 2013521139 A JP2013521139 A JP 2013521139A JP 2013521139 A JP2013521139 A JP 2013521139A JP 2013535460 A5 JP2013535460 A5 JP 2013535460A5
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- trans
- methyl
- cyclopropyl
- amine
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 46
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 28
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 23
- 125000000217 alkyl group Chemical group 0.000 claims 22
- 239000008194 pharmaceutical composition Substances 0.000 claims 18
- 125000001424 substituent group Chemical group 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 13
- 239000012453 solvate Substances 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 11
- 125000004122 cyclic group Chemical group 0.000 claims 10
- 208000012902 Nervous system disease Diseases 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- -1 C-amide Chemical group 0.000 claims 6
- 208000025966 Neurological disease Diseases 0.000 claims 6
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 6
- 230000002265 prevention Effects 0.000 claims 6
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- 125000000335 thiazolyl group Chemical group 0.000 claims 5
- 208000036142 Viral infection Diseases 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 230000009385 viral infection Effects 0.000 claims 4
- HJWZUPRHNBJKHE-VQTJNVASSA-N 5-[[[(1r,2s)-2-(4-phenylmethoxyphenyl)cyclopropyl]amino]methyl]pyrimidin-2-amine Chemical compound C1=NC(N)=NC=C1CN[C@H]1[C@H](C=2C=CC(OCC=3C=CC=CC=3)=CC=2)C1 HJWZUPRHNBJKHE-VQTJNVASSA-N 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 125000001475 halogen functional group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- RAIPHJJURHTUIC-UHFFFAOYSA-N 1,3-thiazol-2-amine Chemical compound NC1=NC=CS1 RAIPHJJURHTUIC-UHFFFAOYSA-N 0.000 claims 2
- VJOTYGQWNUGGSP-DLBZAZTESA-N 5-[[[(1r,2s)-2-(4-phenylmethoxyphenyl)cyclopropyl]amino]methyl]-1,2,4-oxadiazol-3-amine Chemical compound NC1=NOC(CN[C@H]2[C@@H](C2)C=2C=CC(OCC=3C=CC=CC=3)=CC=2)=N1 VJOTYGQWNUGGSP-DLBZAZTESA-N 0.000 claims 2
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 2
- 208000023105 Huntington disease Diseases 0.000 claims 2
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 150000001408 amides Chemical class 0.000 claims 2
- 239000004202 carbamide Substances 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 125000004474 heteroalkylene group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 229940124530 sulfonamide Drugs 0.000 claims 2
- 150000003456 sulfonamides Chemical class 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000004306 triazinyl group Chemical group 0.000 claims 2
- IAXWZYXUKABJAN-UHFFFAOYSA-N 1,2-oxazol-5-amine Chemical compound NC1=CC=NO1 IAXWZYXUKABJAN-UHFFFAOYSA-N 0.000 claims 1
- APKZPKINPXTSNL-UHFFFAOYSA-N 1,3,4-oxadiazol-2-amine Chemical compound NC1=NN=CO1 APKZPKINPXTSNL-UHFFFAOYSA-N 0.000 claims 1
- YBEAMOBHNFDQMM-UHFFFAOYSA-N 1,3-oxazol-5-amine Chemical compound NC1=CN=CO1 YBEAMOBHNFDQMM-UHFFFAOYSA-N 0.000 claims 1
- LKFXYYLRIUSARI-UHFFFAOYSA-N 1,3-thiazol-5-amine Chemical compound NC1=CN=CS1 LKFXYYLRIUSARI-UHFFFAOYSA-N 0.000 claims 1
- JVVRJMXHNUAPHW-UHFFFAOYSA-N 1h-pyrazol-5-amine Chemical compound NC=1C=CNN=1 JVVRJMXHNUAPHW-UHFFFAOYSA-N 0.000 claims 1
- ICSNLGPSRYBMBD-UHFFFAOYSA-N 2-aminopyridine Chemical compound NC1=CC=CC=N1 ICSNLGPSRYBMBD-UHFFFAOYSA-N 0.000 claims 1
- MCRPCHPLDTWWIQ-ZWKOTPCHSA-N 3-[4-[(1s,2r)-2-[(2-amino-1,3-thiazol-5-yl)methylamino]cyclopropyl]phenyl]phenol Chemical compound S1C(N)=NC=C1CN[C@H]1[C@H](C=2C=CC(=CC=2)C=2C=C(O)C=CC=2)C1 MCRPCHPLDTWWIQ-ZWKOTPCHSA-N 0.000 claims 1
- LHGWKSSSHJWPDK-RBUKOAKNSA-N 3-[4-[(1s,2r)-2-[(2-aminopyrimidin-5-yl)methylamino]cyclopropyl]phenyl]phenol Chemical compound C1=NC(N)=NC=C1CN[C@H]1[C@H](C=2C=CC(=CC=2)C=2C=C(O)C=CC=2)C1 LHGWKSSSHJWPDK-RBUKOAKNSA-N 0.000 claims 1
- QNMAQELYEAAQOX-DOTOQJQBSA-N 3-[5-[(1s,2r)-2-[(2-amino-1,3-thiazol-5-yl)methylamino]cyclopropyl]pyridin-2-yl]phenol Chemical compound S1C(N)=NC=C1CN[C@H]1[C@H](C=2C=NC(=CC=2)C=2C=C(O)C=CC=2)C1 QNMAQELYEAAQOX-DOTOQJQBSA-N 0.000 claims 1
- HQKNDJJROYDZDO-FUHWJXTLSA-N 3-[5-[(1s,2r)-2-[(2-aminopyrimidin-5-yl)methylamino]cyclopropyl]pyridin-2-yl]phenol Chemical compound C1=NC(N)=NC=C1CN[C@H]1[C@H](C=2C=NC(=CC=2)C=2C=C(O)C=CC=2)C1 HQKNDJJROYDZDO-FUHWJXTLSA-N 0.000 claims 1
- CNPURSDMOWDNOQ-UHFFFAOYSA-N 4-methoxy-7h-pyrrolo[2,3-d]pyrimidin-2-amine Chemical compound COC1=NC(N)=NC2=C1C=CN2 CNPURSDMOWDNOQ-UHFFFAOYSA-N 0.000 claims 1
- QGMWIWDQYKVIAH-JKSUJKDBSA-N 5-[[[(1R,2S)-2-(4-phenylphenyl)cyclopropyl]amino]methyl]-1,3,4-oxadiazol-2-amine Chemical compound NC1=NN=C(O1)CN[C@H]1[C@@H](C1)C1=CC=C(C=C1)C1=CC=CC=C1 QGMWIWDQYKVIAH-JKSUJKDBSA-N 0.000 claims 1
- UKYBJIFGAZGUOR-RBUKOAKNSA-N 5-[[[(1r,2s)-2-(4-phenylmethoxyphenyl)cyclopropyl]amino]methyl]-1,3-thiazol-2-amine Chemical compound S1C(N)=NC=C1CN[C@H]1[C@H](C=2C=CC(OCC=3C=CC=CC=3)=CC=2)C1 UKYBJIFGAZGUOR-RBUKOAKNSA-N 0.000 claims 1
- LXRJIMUKGUKNSO-FUHWJXTLSA-N 5-[[[(1r,2s)-2-[6-[3-(trifluoromethyl)phenyl]pyridin-3-yl]cyclopropyl]amino]methyl]pyrimidin-2-amine Chemical compound C1=NC(N)=NC=C1CN[C@H]1[C@H](C=2C=NC(=CC=2)C=2C=C(C=CC=2)C(F)(F)F)C1 LXRJIMUKGUKNSO-FUHWJXTLSA-N 0.000 claims 1
- BVFHICUEGWUGBY-RBUKOAKNSA-N 6-[[[(1r,2s)-2-(4-phenylmethoxyphenyl)cyclopropyl]amino]methyl]-1,2,4-triazin-3-amine Chemical compound N1=NC(N)=NC=C1CN[C@H]1[C@H](C=2C=CC(OCC=3C=CC=CC=3)=CC=2)C1 BVFHICUEGWUGBY-RBUKOAKNSA-N 0.000 claims 1
- KOEMDMRKTBTNRR-VQTJNVASSA-N 6-[[[(1r,2s)-2-(4-phenylmethoxyphenyl)cyclopropyl]amino]methyl]pyridazin-3-amine Chemical compound N1=NC(N)=CC=C1CN[C@H]1[C@H](C=2C=CC(OCC=3C=CC=CC=3)=CC=2)C1 KOEMDMRKTBTNRR-VQTJNVASSA-N 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 206010067889 Dementia with Lewy bodies Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 208000029433 Herpesviridae infectious disease Diseases 0.000 claims 1
- 201000002832 Lewy body dementia Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 241000700605 Viruses Species 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 238000011534 incubation Methods 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- XFTQRUTUGRCSGO-UHFFFAOYSA-N pyrazin-2-amine Chemical compound NC1=CN=CC=N1 XFTQRUTUGRCSGO-UHFFFAOYSA-N 0.000 claims 1
- LJXQPZWIHJMPQQ-UHFFFAOYSA-N pyrimidin-2-amine Chemical compound NC1=NC=CC=N1 LJXQPZWIHJMPQQ-UHFFFAOYSA-N 0.000 claims 1
- FVLAYJRLBLHIPV-UHFFFAOYSA-N pyrimidin-5-amine Chemical compound NC1=CN=CN=C1 FVLAYJRLBLHIPV-UHFFFAOYSA-N 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 230000007420 reactivation Effects 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 241001529453 unidentified herpesvirus Species 0.000 claims 1
- XBBRLCXCBCZIOI-DLBZAZTESA-N vafidemstat Chemical compound O1C(N)=NN=C1CN[C@H]1[C@H](C=2C=CC(OCC=3C=CC=CC=3)=CC=2)C1 XBBRLCXCBCZIOI-DLBZAZTESA-N 0.000 claims 1
- 230000007419 viral reactivation Effects 0.000 claims 1
- 125000003368 amide group Chemical group 0.000 description 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 2
- 0 *C(C1)C1NCP Chemical compound *C(C1)C1NCP 0.000 description 1
- 125000004442 acylamino group Chemical group 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10171342 | 2010-07-29 | ||
| EP10171342.8 | 2010-07-29 | ||
| EP11160731.3 | 2011-03-31 | ||
| EP11160738 | 2011-03-31 | ||
| EP11160728.9 | 2011-03-31 | ||
| EP11160728 | 2011-03-31 | ||
| EP11160731 | 2011-03-31 | ||
| EP11160738.8 | 2011-03-31 | ||
| PCT/EP2011/062949 WO2012013728A1 (en) | 2010-07-29 | 2011-07-27 | Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016186185A Division JP2017039740A (ja) | 2010-07-29 | 2016-09-23 | Ｌｓｄ１のアリールシクロプロピルアミンをベースとしたデメチラーゼ阻害剤およびそれらの医学的使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013535460A JP2013535460A (ja) | 2013-09-12 |
| JP2013535460A5 true JP2013535460A5 (OSRAM) | 2014-09-11 |
| JP6054868B2 JP6054868B2 (ja) | 2016-12-27 |
Family
ID=44514682
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013521139A Active JP6054868B2 (ja) | 2010-07-29 | 2011-07-27 | Ｌｓｄ１のアリールシクロプロピルアミンをベースとしたデメチラーゼ阻害剤およびそれらの医学的使用 |
| JP2016186185A Pending JP2017039740A (ja) | 2010-07-29 | 2016-09-23 | Ｌｓｄ１のアリールシクロプロピルアミンをベースとしたデメチラーゼ阻害剤およびそれらの医学的使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016186185A Pending JP2017039740A (ja) | 2010-07-29 | 2016-09-23 | Ｌｓｄ１のアリールシクロプロピルアミンをベースとしたデメチラーゼ阻害剤およびそれらの医学的使用 |
Country Status (26)
| Country | Link |
|---|---|
| US (3) | US9181198B2 (OSRAM) |
| EP (2) | EP2598482B1 (OSRAM) |
| JP (2) | JP6054868B2 (OSRAM) |
| KR (1) | KR101866858B1 (OSRAM) |
| CN (2) | CN103124724B (OSRAM) |
| AU (1) | AU2011284688B2 (OSRAM) |
| BR (1) | BR112013002164B1 (OSRAM) |
| CA (1) | CA2806008C (OSRAM) |
| CY (1) | CY1120586T1 (OSRAM) |
| DK (1) | DK2598482T3 (OSRAM) |
| ES (1) | ES2674747T3 (OSRAM) |
| HR (1) | HRP20180916T1 (OSRAM) |
| HU (1) | HUE037937T2 (OSRAM) |
| IL (1) | IL224389A (OSRAM) |
| LT (1) | LT2598482T (OSRAM) |
| ME (1) | ME03085B (OSRAM) |
| MX (1) | MX341732B (OSRAM) |
| NO (1) | NO2598482T3 (OSRAM) |
| PL (1) | PL2598482T3 (OSRAM) |
| PT (1) | PT2598482T (OSRAM) |
| RS (1) | RS57331B1 (OSRAM) |
| RU (1) | RU2611437C2 (OSRAM) |
| SI (1) | SI2598482T1 (OSRAM) |
| SM (1) | SMT201800323T1 (OSRAM) |
| TR (1) | TR201809057T4 (OSRAM) |
| WO (1) | WO2012013728A1 (OSRAM) |
Families Citing this family (80)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010043721A1 (en) | 2008-10-17 | 2010-04-22 | Oryzon Genomics, S.A. | Oxidase inhibitors and their use |
| EP2389362B1 (en) | 2009-01-21 | 2019-12-11 | Oryzon Genomics, S.A. | Phenylcyclopropylamine derivatives and their medical use |
| BR112012006572A2 (pt) | 2009-09-25 | 2016-04-26 | Oryzon Genomics Sa | inibidores de demetilase-1 de lisina específicos e seu uso |
| EP2486002B1 (en) | 2009-10-09 | 2019-03-27 | Oryzon Genomics, S.A. | Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use |
| WO2011106106A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae |
| US9616058B2 (en) | 2010-02-24 | 2017-04-11 | Oryzon Genomics, S.A. | Potent selective LSD1 inhibitors and dual LSD1/MAO-B inhibitors for antiviral use |
| JP5868948B2 (ja) | 2010-04-19 | 2016-02-24 | オリゾン・ジェノミックス・ソシエダッド・アノニマＯｒｙｚｏｎ Ｇｅｎｏｍｉｃｓ Ｓ．Ａ． | リジン特異的脱メチル化酵素１阻害薬およびその使用 |
| ES2674747T3 (es) * | 2010-07-29 | 2018-07-03 | Oryzon Genomics, S.A. | Inhibidores de demetilasa LSD1 basados en arilciclopropilamina y sus usos médicos |
| US9006449B2 (en) | 2010-07-29 | 2015-04-14 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as LSD1 inhibitors |
| WO2012045883A1 (en) | 2010-10-08 | 2012-04-12 | Oryzon Genomics S.A. | Cyclopropylamine inhibitors of oxidases |
| WO2012072713A2 (en) | 2010-11-30 | 2012-06-07 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae |
| EP3981395A1 (en) | 2011-02-08 | 2022-04-13 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
| US20140163041A1 (en) | 2011-02-08 | 2014-06-12 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders |
| PH12013501871A1 (en) | 2011-03-25 | 2019-06-03 | Glaxosmithkline Ip No 2 Ltd | Cyclopropylamines as lsd1 inhibitors |
| US20140329833A1 (en) | 2011-05-19 | 2014-11-06 | Oryzon Genomics, S.A | Lysine demethylase inhibitors for inflammatory diseases or conditions |
| US20140296255A1 (en) | 2011-05-19 | 2014-10-02 | Oryzong Genomics, S.A. | Lysine demethylase inhibitors for thrombosis and cardiovascular diseases |
| RU2668952C2 (ru) | 2011-10-20 | 2018-10-05 | Оризон Дженомикс, С.А. | (гетеро)арилциклопропиламины в качестве ингибиторов lsd1 |
| EP2768805B1 (en) * | 2011-10-20 | 2020-03-25 | Oryzon Genomics, S.A. | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors |
| WO2014058071A1 (ja) * | 2012-10-12 | 2014-04-17 | 武田薬品工業株式会社 | シクロプロパンアミン化合物およびその用途 |
| CN102863341B (zh) * | 2012-10-22 | 2014-05-07 | 南通大学 | 一种（1r,2s）-2-芳基环丙胺衍生物的化学合成方法 |
| EP2740474A1 (en) | 2012-12-05 | 2014-06-11 | Instituto Europeo di Oncologia S.r.l. | Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a |
| WO2014194280A2 (en) * | 2013-05-30 | 2014-12-04 | The Board of Regents of the Nevada System of Higher Education on behalf of the University of | Novel suicidal lsd1 inhibitors targeting sox2-expressing cancer cells |
| WO2015021128A1 (en) | 2013-08-06 | 2015-02-12 | Imago Biosciences Inc. | Kdm1a inhibitors for the treatment of disease |
| WO2015123437A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| WO2015123408A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| US9670210B2 (en) | 2014-02-13 | 2017-06-06 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| TWI720451B (zh) | 2014-02-13 | 2021-03-01 | 美商英塞特控股公司 | 作為lsd1抑制劑之環丙胺 |
| US9487511B2 (en) | 2014-04-11 | 2016-11-08 | Takeda Pharmaceutical Company Limited | Cyclopropanamine compound and use thereof |
| TWI687419B (zh) | 2014-07-10 | 2020-03-11 | 美商英塞特公司 | 作為ｌｓｄ１抑制劑之咪唑并吡啶及咪唑并吡嗪 |
| WO2016007736A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyrazines as lsd1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| EP3185858A4 (en) | 2014-08-25 | 2017-12-27 | University of Canberra | Compositions for modulating cancer stem cells and uses therefor |
| EA039196B1 (ru) * | 2014-10-08 | 2021-12-16 | Инсайт Корпорейшн | Циклопропиламины в качестве ингибиторов lsd1 |
| CN107438593B (zh) * | 2015-01-30 | 2020-10-30 | 基因泰克公司 | 治疗化合物及其用途 |
| HRP20250119T1 (hr) | 2015-02-12 | 2025-03-28 | Imago Biosciences Inc. | Kdm1a inhibitor i njegova primjena u terapiji |
| MX373154B (es) | 2015-04-03 | 2020-04-22 | Incyte Holdings Corp | Compuestos heterocíclicos como inhibidores de demetilasa 1 específica de lisina (lsd1). |
| EP3090998A1 (en) | 2015-05-06 | 2016-11-09 | F. Hoffmann-La Roche AG | Solid forms |
| CA2987876A1 (en) | 2015-06-12 | 2016-12-15 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| WO2017013061A1 (en) | 2015-07-17 | 2017-01-26 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| LT3334709T (lt) | 2015-08-12 | 2025-03-10 | Incyte Holdings Corporation | Lsd1 inhibitoriaus druskos |
| US10059668B2 (en) | 2015-11-05 | 2018-08-28 | Mirati Therapeutics, Inc. | LSD1 inhibitors |
| PL3381896T3 (pl) | 2015-11-27 | 2023-05-08 | Taiho Pharmaceutical Co., Ltd. | Związek bifenylowy lub jego sól |
| WO2017109061A1 (en) * | 2015-12-23 | 2017-06-29 | Ieo - Istituto Europeo Di Oncologia S.R.L. | Spirocyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a |
| SG11201805645QA (en) | 2015-12-29 | 2018-07-30 | Mirati Therapeutics Inc | Lsd1 inhibitors |
| CN107176927B (zh) * | 2016-03-12 | 2020-02-18 | 福建金乐医药科技有限公司 | 组蛋白去甲基化酶lsd1抑制剂 |
| EA201892075A1 (ru) | 2016-03-15 | 2019-04-30 | Оризон Дженомикс, С.А. | Комбинации ингибиторов lsd1 для применения для лечения солидных опухолей |
| CA3253937A1 (en) | 2016-03-15 | 2025-03-04 | Oryzon Genomics, S.A. | Combinations of Lysine-Specific Demethylase 1 Inhibitors for the Treatment of Hematological Maligna |
| US11034991B2 (en) | 2016-03-16 | 2021-06-15 | Oryzon Genomics S.A. | Methods to determine KDM1A target engagement and chemoprobes useful therefor |
| CN107200706A (zh) | 2016-03-16 | 2017-09-26 | 中国科学院上海药物研究所 | 一类氟取代的环丙胺类化合物及其制备方法、药物组合物和用途 |
| UA125559C2 (uk) | 2016-04-22 | 2022-04-20 | Інсайт Корпорейшн | Композиції інгібітора lsd1 |
| ES2732669T3 (es) | 2016-06-10 | 2019-11-25 | Oryzon Genomics Sa | Tratamiento de la esclerosis múltiple |
| CN111194306B (zh) | 2016-08-16 | 2023-05-16 | 伊美格生物科学公司 | 用于制备kdm1a抑制剂的方法和过程 |
| WO2018083189A1 (en) | 2016-11-03 | 2018-05-11 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| WO2018091691A1 (en) * | 2016-11-17 | 2018-05-24 | Cytoo | Lsd1 inhibitors as skeletal muscle hypertrophy inducers |
| MA51507A (fr) | 2016-12-09 | 2020-11-11 | Constellation Pharmaceuticals Inc | Marqueurs pour un traitement personnalisé du cancer avec des inhibiteurs de lsd1 |
| CA3056527A1 (en) * | 2017-01-24 | 2018-08-02 | Medshine Discovery Inc. | Lsd1 inhibitor and preparation method and application thereof |
| CA3065077C (en) | 2017-05-26 | 2022-09-20 | Taiho Pharmaceutical Co., Ltd. | Novel biphenyl compound or salt thereof |
| MA50467A (fr) | 2017-05-26 | 2020-09-02 | Taiho Pharmaceutical Co Ltd | Potentialisateur d'effet antitumoral utilisant un nouveau composé biphényle |
| US12435128B2 (en) | 2017-05-31 | 2025-10-07 | Taiho Pharmaceutical Co., Ltd. | Method for predicting therapeutic effect of LSD1 inhibitor based on expression of INSM1 |
| JP2020152641A (ja) * | 2017-07-07 | 2020-09-24 | 国立研究開発法人理化学研究所 | リジン特異的脱メチル化酵素１阻害活性を有する新規化合物、その製造方法及びその用途 |
| LT3661510T (lt) * | 2017-08-03 | 2025-01-27 | Oryzon Genomics, S.A. | Elgesio pakitimų gydymo būdai |
| WO2019068326A1 (en) | 2017-10-05 | 2019-04-11 | Université D'aix-Marseille | INHIBITORS OF LSD1 FOR THE TREATMENT AND PREVENTION OF CARDIOMYOPATHIES |
| US11578059B2 (en) | 2018-05-11 | 2023-02-14 | Imago Biosciences. Inc. | KDM1A inhibitors for the treatment of disease |
| JP7358466B2 (ja) * | 2018-07-20 | 2023-10-10 | 石薬集団中奇制薬技術（石家荘）有限公司 | Ｌｓｄ１阻害剤の塩及びその結晶型 |
| US10968200B2 (en) | 2018-08-31 | 2021-04-06 | Incyte Corporation | Salts of an LSD1 inhibitor and processes for preparing the same |
| CN112672994B (zh) * | 2018-09-13 | 2022-09-13 | 南昌弘益药业有限公司 | 作为lsd1抑制剂的杂螺环类化合物及其应用 |
| SG11202109159VA (en) | 2019-03-20 | 2021-10-28 | Oryzon Genomics Sa | Methods of treating borderline personality disorder |
| CN120837494A (zh) | 2019-03-20 | 2025-10-28 | 奥莱松基因组股份有限公司 | 使用kdm1a抑制剂如化合物伐菲德司他治疗注意缺陷多动症的方法 |
| WO2021004610A1 (en) | 2019-07-05 | 2021-01-14 | Oryzon Genomics, S.A. | Biomarkers and methods for personalized treatment of small cell lung cancer using kdm1a inhibitors |
| CN114615979A (zh) | 2019-09-03 | 2022-06-10 | 奥莱松基因组股份有限公司 | 用于治疗孤独症谱系障碍的伐菲德司他 |
| BR112022008020A2 (pt) | 2019-11-13 | 2022-07-12 | Taiho Pharmaceutical Co Ltd | Métodos de tratamento de doenças e distúrbios relacionados a lsd1 com inibidores de lsd1 |
| IT202000007873A1 (it) | 2020-04-14 | 2021-10-14 | St Europeo Di Oncologia S R L | Molecole per uso nel trattamento delle infezioni virali |
| WO2021228146A1 (zh) * | 2020-05-12 | 2021-11-18 | 石药集团中奇制药技术（石家庄）有限公司 | 一种lsd1抑制剂的用途 |
| EP3964204A1 (en) | 2020-09-08 | 2022-03-09 | Université d'Aix-Marseille | Lsd1 inhibitors for use in the treatment and prevention of fibrosis of tissues |
| KR20230167102A (ko) | 2021-04-08 | 2023-12-07 | 오리존 지노믹스 에스.에이. | 골수성 암 치료를 위한 lsd1 억제제의 조합물 |
| CN113582906B (zh) * | 2021-08-24 | 2023-05-16 | 郑州大学 | 二氟苯环丙胺类化合物及其制备方法和应用 |
| JP2025516648A (ja) | 2022-05-09 | 2025-05-30 | オリゾン・ゲノミクス・ソシエダッド・アノニマ | Ｌｓｄ１阻害薬を用いるｎｆ１変異腫瘍の治療法 |
| WO2023217758A1 (en) | 2022-05-09 | 2023-11-16 | Oryzon Genomics, S.A. | Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors |
| WO2024110649A1 (en) | 2022-11-24 | 2024-05-30 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors and menin inhibitors for treating cancer |
Family Cites Families (131)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3106578A (en) | 1960-09-16 | 1963-10-08 | Smith Kline French Lab | Nu-phenethyl-2-phenylcyclopropylamine derivatives |
| US3365458A (en) | 1964-06-23 | 1968-01-23 | Aldrich Chem Co Inc | N-aryl-n'-cyclopropyl-ethylene diamine derivatives |
| US3532749A (en) | 1965-05-11 | 1970-10-06 | Aldrich Chem Co Inc | N'-propargyl-n**2-cyclopropyl-ethylenediamines and the salts thereof |
| US3471522A (en) | 1967-09-29 | 1969-10-07 | Aldrich Chem Co Inc | N-cyclopropyl-n'-furfuryl-n'-methyl ethylene diamines |
| US3532712A (en) | 1967-09-29 | 1970-10-06 | Aldrich Chem Co Inc | N'-cyclopropyl ethylenediamine derivatives |
| US3654306A (en) | 1970-01-26 | 1972-04-04 | Robins Co Inc A H | 5-azaspiro(2.4)heptane-4 6-diones |
| US3758684A (en) | 1971-09-07 | 1973-09-11 | Burroughs Wellcome Co | Treating dna virus infections with amino purine derivatives |
| US4530901A (en) | 1980-01-08 | 1985-07-23 | Biogen N.V. | Recombinant DNA molecules and their use in producing human interferon-like polypeptides |
| US4409243A (en) | 1981-11-09 | 1983-10-11 | Julian Lieb | Treatment of auto-immune and inflammatory diseases |
| US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
| GB9311282D0 (en) | 1993-06-01 | 1993-07-21 | Rhone Poulenc Rorer Ltd | New compositions of matter |
| DE69535461T2 (de) | 1994-10-21 | 2008-09-25 | NPS Pharmaceuticals, Inc., Salt Lake City | Kalzium-rezeptor aktive verbindungen |
| US5652258A (en) | 1995-05-30 | 1997-07-29 | Gliatech, Inc. | 2-(4-imidazoyl) cyclopropyl derivatives |
| US20040132820A1 (en) | 1996-02-15 | 2004-07-08 | Jean Gosselin | Agents with leukotriene B4-like antiviral (DNA) and anti-neoplastic activities |
| GB9615730D0 (en) | 1996-07-26 | 1996-09-04 | Medical Res Council | Anti-viral agent 1 |
| US5961987A (en) | 1996-10-31 | 1999-10-05 | University Of Iowa Research Foundation | Ocular protein stimulants |
| DE19647615A1 (de) | 1996-11-18 | 1998-05-20 | Bayer Ag | Verfahren zur Herstellung von Cyclopropylaminen |
| TW530058B (en) | 1997-07-22 | 2003-05-01 | Astra Pharma Prod | Triazolo [4,5-d]pyrimidine compounos and their use and process for preparation |
| SE9702772D0 (sv) | 1997-07-22 | 1997-07-22 | Astra Pharma Prod | Novel compounds |
| AU1631699A (en) | 1997-12-18 | 1999-07-05 | E.I. Du Pont De Nemours And Company | Cyclohexylamine arthropodicides and fungicides |
| US6809120B1 (en) | 1998-01-13 | 2004-10-26 | University Of Saskatchewan Technologies Inc. | Composition containing propargylamine for enhancing cancer therapy |
| US6486183B1 (en) * | 1998-01-16 | 2002-11-26 | Medivir Ab | Antivirals |
| WO1999054440A1 (en) | 1998-04-21 | 1999-10-28 | Micromet Gesellschaft Für Biomedizinische Forschung Mbh | CD19xCD3 SPECIFIC POLYPEPTIDES AND USES THEREOF |
| SE9802206D0 (sv) | 1998-06-22 | 1998-06-22 | Astra Pharma Inc | Novel compounds |
| GB2344337A (en) | 1998-12-02 | 2000-06-07 | Fcp | Carton having a rim |
| TWI229674B (en) | 1998-12-04 | 2005-03-21 | Astra Pharma Prod | Novel triazolo[4,5-d]pyrimidine compounds, pharmaceutical composition containing the same, their process for preparation and uses |
| IL152726A0 (en) | 2000-05-26 | 2003-06-24 | Schering Corp | Adenosine a2a receptor antagonists |
| TWI290549B (en) * | 2000-06-02 | 2007-12-01 | Astrazeneca Ab | Process for the preparation of cyclopropyl carboxylic acid ester and derivatives |
| JP2001354563A (ja) | 2000-06-09 | 2001-12-25 | Sankyo Co Ltd | 置換ベンジルアミン類を含有する医薬 |
| US8519005B2 (en) | 2000-07-27 | 2013-08-27 | Thomas N. Thomas | Compositions and methods to prevent toxicity of antiinflammatory agents and enhance their efficacy |
| EP1193268A1 (en) | 2000-09-27 | 2002-04-03 | Applied Research Systems ARS Holding N.V. | Pharmaceutically active sulfonamide derivatives bearing both lipophilic and ionisable moieties as inhibitors of protein Junkinases |
| WO2002068415A1 (en) | 2000-12-21 | 2002-09-06 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| EP1373203A1 (en) | 2001-03-29 | 2004-01-02 | Bristol-Myers Squibb Company | Cyclopropylindole derivatives as selective serotonin reuptake inhibitors |
| RU2332415C2 (ru) | 2001-04-27 | 2008-08-27 | Вертекс Фармасьютикалз Инкорпорейтед | Производные пиразола, полезные в качестве ингибиторов протеинкиназы |
| DE10123163A1 (de) | 2001-05-09 | 2003-01-16 | Gruenenthal Gmbh | Substituierte Cyclohexan-1,4-diaminderivate |
| US20030008844A1 (en) | 2001-05-17 | 2003-01-09 | Keryx Biopharmaceuticals, Inc. | Use of sulodexide for the treatment of inflammatory bowel disease |
| EP1499598A1 (en) | 2002-04-18 | 2005-01-26 | Ucb, S.A. | Chemical compounds with dual activity, processes for their preparation and pharmaceutical compositions |
| US7704995B2 (en) | 2002-05-03 | 2010-04-27 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| WO2003093297A2 (en) | 2002-05-03 | 2003-11-13 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| US7312214B2 (en) | 2002-05-10 | 2007-12-25 | Bristol-Myers Squibb Company | 1, 1-disubstituted cycloalkyl derivatives as factor Xa inhibitors |
| US6951961B2 (en) | 2002-05-17 | 2005-10-04 | Marina Nikolaevna Protopopova | Methods of use and compositions for the diagnosis and treatment of infectious disease |
| US20040033986A1 (en) | 2002-05-17 | 2004-02-19 | Protopopova Marina Nikolaevna | Anti tubercular drug: compositions and methods |
| US7456222B2 (en) | 2002-05-17 | 2008-11-25 | Sequella, Inc. | Anti tubercular drug: compositions and methods |
| ES2361011T3 (es) | 2002-05-20 | 2011-06-13 | Bristol-Myers Squibb Company | Inhibidores del virus de la hepatitis c. |
| US7611704B2 (en) | 2002-07-15 | 2009-11-03 | Board Of Regents, The University Of Texas System | Compositions and methods for treating viral infections using antibodies and immunoconjugates to aminophospholipids |
| SE0202539D0 (sv) | 2002-08-27 | 2002-08-27 | Astrazeneca Ab | Compounds |
| DE60318891T2 (de) | 2002-12-13 | 2009-01-22 | Smithkline Beecham Corp. | Cyclopropylverbindungen als ccr5 antagonisten |
| SG2012000667A (en) | 2003-01-08 | 2015-03-30 | Univ Washington | Antibacterial agents |
| US7223785B2 (en) | 2003-01-22 | 2007-05-29 | Boehringer Ingelheim International Gmbh | Viral polymerase inhibitors |
| GB0303439D0 (en) | 2003-02-14 | 2003-03-19 | Pfizer Ltd | Antiparasitic terpene alkaloids |
| US7186832B2 (en) | 2003-02-20 | 2007-03-06 | Sugen Inc. | Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors |
| US7135575B2 (en) | 2003-03-03 | 2006-11-14 | Array Biopharma, Inc. | P38 inhibitors and methods of use thereof |
| EP1631548B1 (en) | 2003-04-24 | 2009-10-28 | Merck & Co., Inc. | Inhibitors of akt activity |
| CA2529036A1 (en) | 2003-07-03 | 2005-02-03 | Eli Lilly And Company | Indane derivates as muscarinic receptor agonists |
| CN102060806A (zh) | 2003-09-11 | 2011-05-18 | iTherX药品公司 | 细胞因子抑制剂 |
| EP1663193B1 (en) | 2003-09-12 | 2012-04-04 | Merck Serono SA | Sulfonamide derivatives for the treatment of diabetes |
| CN1897950A (zh) | 2003-10-14 | 2007-01-17 | 惠氏公司 | 稠合芳基和杂芳基衍生物及其使用方法 |
| EP1677799A4 (en) | 2003-10-21 | 2008-09-10 | Merck & Co Inc | TRIAZOLO-PYRIDAZINE COMPOUNDS AND DERIVATIVES THEREOF FOR THE TREATMENT OF NEUROPATHIC PAIN |
| US7026339B2 (en) | 2003-11-07 | 2006-04-11 | Fan Yang | Inhibitors of HCV NS5B polymerase |
| WO2005058808A1 (en) | 2003-12-15 | 2005-06-30 | Japan Tobacco Inc. | N-substituted-n-sulfonylaminocyclopropane compounds and pharmaceutical use thereof |
| AU2004299461A1 (en) | 2003-12-15 | 2005-06-30 | Almirall Ag | 2, 6 bisheteroaryl-4-aminopyrimidines as adenosine receptor antagonists |
| CN1901971A (zh) | 2003-12-15 | 2007-01-24 | 日本烟草产业株式会社 | 环丙烷化合物及其药物应用 |
| US7399825B2 (en) | 2003-12-24 | 2008-07-15 | Lipps Binie V | Synthetic peptide, inhibitor to DNA viruses |
| CA2564356A1 (en) | 2004-04-26 | 2005-11-03 | Pfizer Inc. | Pyrrolopyridine derivatives and their use as hiv-integrase inhibitors |
| US20090275099A1 (en) | 2004-04-27 | 2009-11-05 | Regents Of The University Of Michigan | Methods and compositions for treating diseases and conditions associated with mitochondrial function |
| CN1950326A (zh) * | 2004-06-28 | 2007-04-18 | 特瓦药物精化学品股份有限公司 | 托莫西汀的光学拆分和重新利用方法 |
| DE102004057594A1 (de) | 2004-11-29 | 2006-06-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Substitueirte Pteridine zur Behandlung von entzündlichen Erkrankungen |
| AU2005322312B2 (en) | 2004-12-16 | 2011-05-26 | President And Fellows Of Harvard College | Histone demethylation mediated by the nuclear amine oxidase homolog LSD1 |
| DK1704859T3 (da) | 2005-02-18 | 2010-11-22 | Universitaetsklinikum Freiburg | Kontrol af androgen receptor-afhængig genenkspression ved inhibering af amin-oxidase-aktiviteten af lysin-specifik demetylase (LSD1) |
| US20060275366A1 (en) | 2005-06-02 | 2006-12-07 | Schering Corporation | Controlled-release formulation |
| US7273882B2 (en) | 2005-06-21 | 2007-09-25 | Bristol-Myers Squibb Company | Aminoacetamide acyl guanidines as β-secretase inhibitors |
| EP1741708A1 (en) | 2005-06-28 | 2007-01-10 | Sanofi-Aventis Deutschland GmbH | Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals |
| NZ565059A (en) | 2005-07-25 | 2011-08-26 | Intermune Inc | Novel macrocyclic inhibitors of hepatitus C virus replication |
| WO2007021839A2 (en) | 2005-08-10 | 2007-02-22 | Johns Hopkins University | Polyamines useful as anti-parasitic and anti-cancer therapeutics and as lysine-specific demethylase inhibitors |
| US20090203750A1 (en) | 2005-08-24 | 2009-08-13 | Alan Kozikowski | 5-HT2C Receptor Agonists as Anorectic Agents |
| GB0517740D0 (en) | 2005-08-31 | 2005-10-12 | Novartis Ag | Organic compounds |
| TW200745067A (en) | 2006-03-14 | 2007-12-16 | Astrazeneca Ab | Novel compounds |
| DE602007003343D1 (de) | 2006-05-18 | 2009-12-31 | Syngenta Ltd | Neue mikrobiozide |
| US8198301B2 (en) | 2006-07-05 | 2012-06-12 | Hesheng Zhang | Quinazoline and quinoline derivatives as irreversibe protein tyrosine kinase inhibitors |
| CA2658484A1 (en) | 2006-07-20 | 2008-01-24 | Vical Incorporated | Compositions and methods for vaccinating against hsv-2 |
| WO2008033466A2 (en) | 2006-09-14 | 2008-03-20 | Combinatorx (Singapore) Pre. Ltd. | Compositions and methods for treatment of viral diseases |
| US20110092601A1 (en) | 2007-04-13 | 2011-04-21 | The Johns Hopkins University | Lysine-specific demethylase inhibitors |
| US7906513B2 (en) | 2007-04-26 | 2011-03-15 | Enanta Pharmaceuticals, Inc. | Hydrazide-containing hepatitis C serine protease inhibitors |
| BRPI0813244B8 (pt) | 2007-06-27 | 2021-05-25 | Astrazeneca Ab | compostos derivados de pirazinona, composições compreendendo ditos compostos, uso dos compostos no tratamento de doenças de pulmão e composto intermediário |
| MX2010001650A (es) | 2007-08-10 | 2010-08-02 | Glaxosmithkline Llc | Entidades quimicas biciclicas que contienen nitrogeno para el tratamiento de infecciones virales. |
| WO2009039134A1 (en) | 2007-09-17 | 2009-03-26 | Abbott Laboratories | Anti-infective pyrimidines and uses thereof |
| US20100016262A1 (en) | 2007-10-18 | 2010-01-21 | Yale University | Compositions and methods for reducing hepatotoxicity associated with drug administration and treating non-alcoholic fatty liver disease, non-alcoholic steatohepatitis and associated cirrhosis |
| EP2215065B1 (en) | 2007-10-19 | 2012-07-11 | Boehringer Ingelheim International GmbH | Ccr10 antagonists |
| CA2710417A1 (en) | 2007-12-26 | 2009-07-02 | Shionogi & Co., Ltd. | Glycosylated glycopeptide antibiotic derivatives |
| WO2009109991A2 (en) | 2008-01-23 | 2009-09-11 | Sun Pharma Advanced Research Company Ltd., | Novel hydrazide containing tyrosine kinase inhibitors |
| MX2010008202A (es) | 2008-01-28 | 2010-12-06 | Janssen Pharmaceutica Nv | Derivados de tio-2-aminoquinolina 6-sustituida utiles como inhibidores de beta-secretasa (bace). |
| AU2009225647C1 (en) | 2008-03-19 | 2015-11-19 | Aurimmed Pharma, Inc. | Novel compounds advantageous in the treatment of central nervous system diseases and disorders |
| EP2502907B1 (de) | 2008-03-27 | 2018-08-29 | Grünenthal GmbH | Substituierte 4-Aminocyclohexan-Derivate |
| WO2010014921A2 (en) | 2008-08-01 | 2010-02-04 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | A3 adenosine receptor antagonists and partial agonists |
| CA2723205C (en) | 2008-04-16 | 2017-03-14 | Portola Pharmaceuticals, Inc. | 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinase inhibitors |
| EP2303889A1 (en) | 2008-06-18 | 2011-04-06 | F. Hoffmann-La Roche AG | Halo-substituted pyrimidodiazepines as plkl inhibitors |
| EP2317992A2 (en) | 2008-07-24 | 2011-05-11 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Preventing or treating viral infection using an inhibitor of the lsd1 protein, a mao inhibitor or an inhibitor of lsd1 and a mao inhibitor |
| US8048887B2 (en) | 2008-09-11 | 2011-11-01 | Bristol-Myers Squibb Company | Compounds for the treatment of hepatitis C |
| WO2010043721A1 (en) * | 2008-10-17 | 2010-04-22 | Oryzon Genomics, S.A. | Oxidase inhibitors and their use |
| EP2389362B1 (en) | 2009-01-21 | 2019-12-11 | Oryzon Genomics, S.A. | Phenylcyclopropylamine derivatives and their medical use |
| US8299100B2 (en) | 2009-01-23 | 2012-10-30 | Northwestern University | Potent and selective neuronal nitric oxide synthase inhibitors with improved membrane permeability |
| CA2753382C (en) | 2009-02-27 | 2014-12-23 | Enanta Pharmaceuticals, Inc. | Hepatitis c virus inhibitors |
| PT2429995E (pt) | 2009-05-15 | 2014-04-30 | Novartis Ag | Arilpiridinas como inibidores de aldosterona sintase |
| US8389580B2 (en) | 2009-06-02 | 2013-03-05 | Duke University | Arylcyclopropylamines and methods of use |
| EP2258865A1 (en) | 2009-06-05 | 2010-12-08 | Universitätsklinikum Freiburg | Lysine-specific demethylase 1 (LSD1) is a biomarker for breast cancer |
| WO2010143582A1 (ja) | 2009-06-11 | 2010-12-16 | 公立大学法人名古屋市立大学 | フェニルシクロプロピルアミン誘導体及びlsd1阻害剤 |
| US9708255B2 (en) | 2009-08-18 | 2017-07-18 | Robert A. Casero | (bis)urea and (bis)thiourea compounds as epigenic modulators of lysine-specific demethylase 1 and methods of treating disorders |
| WO2011031934A1 (en) | 2009-09-11 | 2011-03-17 | Enanta Pharmaceuticals, Inc. | Hepatitis c virus inhibitors |
| BR112012006572A2 (pt) * | 2009-09-25 | 2016-04-26 | Oryzon Genomics Sa | inibidores de demetilase-1 de lisina específicos e seu uso |
| EP2486002B1 (en) | 2009-10-09 | 2019-03-27 | Oryzon Genomics, S.A. | Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use |
| WO2011057262A2 (en) | 2009-11-09 | 2011-05-12 | Evolva Inc. | Treatment of infections with tp receptor antagonists |
| WO2011106106A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae |
| US9616058B2 (en) | 2010-02-24 | 2017-04-11 | Oryzon Genomics, S.A. | Potent selective LSD1 inhibitors and dual LSD1/MAO-B inhibitors for antiviral use |
| WO2011113005A2 (en) | 2010-03-12 | 2011-09-15 | The Johns Hopkins University | Compositions and methods for combinations of oligoamines with 2-difluoromethylornithine (dfmo) |
| JP5868948B2 (ja) | 2010-04-19 | 2016-02-24 | オリゾン・ジェノミックス・ソシエダッド・アノニマＯｒｙｚｏｎ Ｇｅｎｏｍｉｃｓ Ｓ．Ａ． | リジン特異的脱メチル化酵素１阻害薬およびその使用 |
| EP2560939A2 (en) | 2010-04-20 | 2013-02-27 | Actavis Group Ptc Ehf | Novel process for preparing phenylcyclopropylamine derivatives using novel intermediates |
| US8765820B2 (en) | 2010-04-20 | 2014-07-01 | Universita Degli Studi Di Roma “La Sapienza” | Tranylcypromine derivatives as inhibitors of histone demethylases LSD1 and/or LSD2 |
| US20130165696A1 (en) | 2010-06-30 | 2013-06-27 | Actavis Group Ptc Ehf | Novel processes for the preparation of phenylcyclopropylamine derivatives and use thereof for preparing ticagrelor |
| US9006449B2 (en) | 2010-07-29 | 2015-04-14 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as LSD1 inhibitors |
| ES2674747T3 (es) * | 2010-07-29 | 2018-07-03 | Oryzon Genomics, S.A. | Inhibidores de demetilasa LSD1 basados en arilciclopropilamina y sus usos médicos |
| WO2012034116A2 (en) | 2010-09-10 | 2012-03-15 | The Johns Hopkins University | Small molecules as epigenetic modulators of lysine-specific demethylase 1 and methods of treating disorders |
| US20130303545A1 (en) | 2010-09-30 | 2013-11-14 | Tamara Maes | Cyclopropylamine derivatives useful as lsd1 inhibitors |
| WO2012045883A1 (en) | 2010-10-08 | 2012-04-12 | Oryzon Genomics S.A. | Cyclopropylamine inhibitors of oxidases |
| WO2012072713A2 (en) | 2010-11-30 | 2012-06-07 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae |
| US20140163041A1 (en) | 2011-02-08 | 2014-06-12 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders |
| EP3981395A1 (en) | 2011-02-08 | 2022-04-13 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
| PH12013501871A1 (en) | 2011-03-25 | 2019-06-03 | Glaxosmithkline Ip No 2 Ltd | Cyclopropylamines as lsd1 inhibitors |
| US20140329833A1 (en) | 2011-05-19 | 2014-11-06 | Oryzon Genomics, S.A | Lysine demethylase inhibitors for inflammatory diseases or conditions |
| US20140296255A1 (en) | 2011-05-19 | 2014-10-02 | Oryzong Genomics, S.A. | Lysine demethylase inhibitors for thrombosis and cardiovascular diseases |
| EP2768805B1 (en) | 2011-10-20 | 2020-03-25 | Oryzon Genomics, S.A. | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors |
| RU2668952C2 (ru) | 2011-10-20 | 2018-10-05 | Оризон Дженомикс, С.А. | (гетеро)арилциклопропиламины в качестве ингибиторов lsd1 |
-
2011
- 2011-07-27 ES ES11749119.1T patent/ES2674747T3/es active Active
- 2011-07-27 CN CN201180047286.3A patent/CN103124724B/zh active Active
- 2011-07-27 CA CA2806008A patent/CA2806008C/en active Active
- 2011-07-27 TR TR2018/09057T patent/TR201809057T4/tr unknown
- 2011-07-27 MX MX2013000968A patent/MX341732B/es active IP Right Grant
- 2011-07-27 EP EP11749119.1A patent/EP2598482B1/en active Active
- 2011-07-27 JP JP2013521139A patent/JP6054868B2/ja active Active
- 2011-07-27 RU RU2013108702A patent/RU2611437C2/ru active
- 2011-07-27 BR BR112013002164-0A patent/BR112013002164B1/pt active IP Right Grant
- 2011-07-27 EP EP18165419.5A patent/EP3375775A1/en not_active Withdrawn
- 2011-07-27 WO PCT/EP2011/062949 patent/WO2012013728A1/en not_active Ceased
- 2011-07-27 HU HUE11749119A patent/HUE037937T2/hu unknown
- 2011-07-27 KR KR1020137004877A patent/KR101866858B1/ko active Active
- 2011-07-27 RS RS20180684A patent/RS57331B1/sr unknown
- 2011-07-27 DK DK11749119.1T patent/DK2598482T3/en active
- 2011-07-27 PL PL11749119T patent/PL2598482T3/pl unknown
- 2011-07-27 ME MEP-2018-163A patent/ME03085B/me unknown
- 2011-07-27 HR HRP20180916TT patent/HRP20180916T1/hr unknown
- 2011-07-27 NO NO11749119A patent/NO2598482T3/no unknown
- 2011-07-27 PT PT117491191T patent/PT2598482T/pt unknown
- 2011-07-27 AU AU2011284688A patent/AU2011284688B2/en active Active
- 2011-07-27 SI SI201131504T patent/SI2598482T1/sl unknown
- 2011-07-27 CN CN201510197250.3A patent/CN104892525A/zh active Pending
- 2011-07-27 LT LTEP11749119.1T patent/LT2598482T/lt unknown
- 2011-07-27 SM SM20180323T patent/SMT201800323T1/it unknown
- 2011-07-27 US US13/812,366 patent/US9181198B2/en active Active
-
2013
- 2013-01-24 IL IL224389A patent/IL224389A/en active IP Right Grant
-
2015
- 2015-09-09 US US14/848,649 patent/US9708309B2/en active Active
-
2016
- 2016-09-23 JP JP2016186185A patent/JP2017039740A/ja active Pending
-
2017
- 2017-06-15 US US15/623,866 patent/US10233178B2/en active Active
-
2018
- 2018-06-22 CY CY181100649T patent/CY1120586T1/el unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013535460A5 (OSRAM) | ||
| HRP20180916T1 (hr) | Inhibitori demetilaze od lsd1 na bazi arilciklopropilamina i njihova medicinska uporaba | |
| JP2008516986A5 (OSRAM) | ||
| JP2016529324A5 (OSRAM) | ||
| ES2675022T3 (es) | Inhibidores de indolamina 2,3-dioxigenasa (IDO) | |
| JP2019529484A5 (OSRAM) | ||
| RU2013143028A (ru) | Тиазолилфенилбензолсульфонамидопроизводные в качестве ингибиторов киназ | |
| JP2011520896A5 (OSRAM) | ||
| US20190345138A1 (en) | Heterocyclic amides as kinase inhibitors | |
| RU2010150786A (ru) | Пирролопиридины как ингибиторы киназы | |
| JP2017526677A5 (OSRAM) | ||
| IL264982B (en) | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors | |
| JP2010540462A5 (OSRAM) | ||
| RU2017121044A (ru) | Производные амидотиадиазола в качестве ингибиторов надфн-оксидазы | |
| JP2019517487A5 (OSRAM) | ||
| JP2019527718A5 (OSRAM) | ||
| JP2017537948A5 (OSRAM) | ||
| JP2015520769A5 (OSRAM) | ||
| JP2016510038A5 (OSRAM) | ||
| JP2008509187A5 (OSRAM) | ||
| JP2012507566A5 (OSRAM) | ||
| CA2582029A1 (en) | Aryl nitrogen-containing bicyclic compounds and methods of use | |
| JP2017508766A5 (OSRAM) | ||
| JP2015524837A5 (OSRAM) | ||
| BR112021005903A2 (pt) | inibidores de vap-1 |